Synthesis and Evaluation of Boron-Containing Heterocyclic Compounds with Antimicrobial and Anticancer Activities

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Prates, Joao Lucas Bruno ; Silva, Samanta de Matos ; Medina-Alarcon, Kaila Petrolina ; dos Santos, Kelvin Sousa ; Belizario, Jenyffie Araujo ; Lopes, Juliana Romano ; Marin-Dett, Freddy Humberto ; Campos, Debora Leite ; Giannini, Maria Jose Soares Mendes ; Fusco-Almeida, Ana Marisa ; Barbugli, Paula Aboud ; Pavan, Fernando Rogerio ; Dos Santos, Jean Leandro

• Document type: Journal article
• Source: Molecules; v. 30, n. 5, p. 27-pg., 2025-03-01.

Abstract

Organoboron compounds, especially those containing boronic acid and benzoxaborole in their structure, have been gaining prominence in medicinal chemistry, following the FDA approval of tavaborole for the treatment of onychomycosis and bortezomib for multiple myeloma. The antimicrobial and anticancer effects of organoboron compounds motivate the investigation of the effects of the novel derivatives described here. A total of fourteen new boronic derivatives were synthesized and characterized using analytical methods. The antimicrobial activities were evaluated against M. tuberculosis (Mtb) H37Rv strains and fungal dermatophytes (C. albicans, ATCC 90028; T. rubrum, ATCC 28189; and T. mentagrophytes, ATCC 11481), while the anticancer effect was evaluated against oral squamous cell carcinoma (SCC) cell lines. Several promising boron-containing prototypes were identified, providing a foundation for further molecular optimization in the development of new antimicrobial and anticancer compounds. (AU)

• FAPESP's process: 22/15826-0 - From the development of three-dimensional human lung models of infection to the evolution of functional human lung models for studying the interaction with Histoplasma capsulatum biofilm
• Grantee: Ana Marisa Fusco Almeida
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• FAPESP's process: 19/07574-9 - The role pattern of biofilm-derived factors in cell signaling: cell death mechanisms and tumorigenic pathways
• Grantee: Paula Aboud Barbugli
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• FAPESP's process: 23/01664-1 - Synthesis and characterization of antimicrobial peptide "B1CTcu5" analogs encapsulated in colon-specific microparticles and in vitro an in vivo studies against Mycobacterium tuberculosis
• Grantee: Fernando Rogério Pavan
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• FAPESP's process: 23/03556-1 - Study of the pathogenesis of mono/polymicrobial dermatophytes biofilms in ex vivo models and application of control strategies.
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• FAPESP's process: 23/05739-6 - Strategies for intervention in gamma-globin gene repressor complexes containing Histone Deacetylase (HDAC-1 and HDAC-2) using small molecules
• Grantee: Jean Leandro dos Santos
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